Synthesis and SAR of novel quinazolines as potent and brain-penetrant c-jun N-terminal kinase (JNK) inhibitors.
Basic Information
ID: ALA1759990
Journal: Bioorg Med Chem Lett
Title: Synthesis and SAR of novel quinazolines as potent and brain-penetrant c-jun N-terminal kinase (JNK) inhibitors.
Authors: He Y, Kamenecka TM, Shin Y, Song X, Jiang R, Noel R, Duckett D, Chen W, Ling YY, Cameron MD, Lin L, Khan S, Koenig M, LoGrasso PV.
Abstract: Quinazoline 3 was discovered as a novel c-jun N-terminal kinase (JNK) inhibitor with good brain penetration and pharmacokinetic (PK) properties. A number of analogs which were potent both in the biochemical and cellular assays were discovered. Quinazoline 13a was found to be a potent JNK3 inhibitor (IC(50)=40 nM), with >500-fold selectivity over p38, and had good PK and brain penetration properties. With these properties, 13a is considered a potential candidate for in vivo evaluation.
CiteXplore: 21316221
DOI: 10.1016/j.bmcl.2011.01.079
Patent ID: ┄